JP2013536876A - 選択性ｃｏｘ−２阻害剤および一酸化窒素ドナーである１，５−ジアリール−２−アルキルピロール−３−置換ニトロエステル - Google Patents

選択性ｃｏｘ−２阻害剤および一酸化窒素ドナーである１，５−ジアリール−２−アルキルピロール−３−置換ニトロエステル Download PDF

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JP2013536876A
JP2013536876A JP2013527725A JP2013527725A JP2013536876A JP 2013536876 A JP2013536876 A JP 2013536876A JP 2013527725 A JP2013527725 A JP 2013527725A JP 2013527725 A JP2013527725 A JP 2013527725A JP 2013536876 A JP2013536876 A JP 2013536876A
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アントニオ・ジョルダーニ
マリアンジェラ・ビアーヴァ
マウリツィオ・アンツィーニ
ヴィンセンツォ・カルデローネ
ルチオ・クラウディオ・ロヴァーティ
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Rottapharm SpA
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D207/30—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members
    • C07D207/32—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
    • C07D207/33—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms with substituted hydrocarbon radicals, directly attached to ring carbon atoms
    • C07D207/337—Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A—HUMAN NECESSITIES
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    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/06—Antipsoriatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00—Drugs for disorders of the muscular or neuromuscular system
    • A61P21/02—Muscle relaxants, e.g. for tetanus or cramps
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/04—Centrally acting analgesics, e.g. opioids
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
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    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D207/30—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members
    • C07D207/32—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
    • C07D207/33—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms with substituted hydrocarbon radicals, directly attached to ring carbon atoms
    • C07D207/333—Radicals substituted by oxygen or sulfur atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D207/30—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members
    • C07D207/32—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
    • C07D207/33—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms with substituted hydrocarbon radicals, directly attached to ring carbon atoms
    • C07D207/335—Radicals substituted by nitrogen atoms not forming part of a nitro radical
    • Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02A—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
    • Y02A50/00—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
    • Y02A50/30—Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
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  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Epidemiology (AREA)
  • Pain & Pain Management (AREA)
  • Immunology (AREA)
  • Neurology (AREA)
  • Rheumatology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Dermatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Pyrrole Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
JP2013527725A 2010-09-07 2011-09-07 選択性ｃｏｘ−２阻害剤および一酸化窒素ドナーである１，５−ジアリール−２−アルキルピロール−３−置換ニトロエステル Withdrawn JP2013536876A (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
ITTO2010A000739 2010-09-07
ITTO2010A000739A IT1402177B1 (it) 2010-09-07 2010-09-07 Nitroesteri di 1,5-diaril-2-alchil-pirroli-3-sostituiti, inibitori selettivi di cox-2 e donatori di ossido nitroso
PCT/IB2011/053914 WO2012032479A1 (en) 2010-09-07 2011-09-07 L,5-diaryl-2-alkvlpvrrole-3-substituted nitro esters, selective cox-2 inhibitors and nitric oxide donors

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Publication Number Publication Date
JP2013536876A true JP2013536876A (ja) 2013-09-26

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JP2013527725A Withdrawn JP2013536876A (ja) 2010-09-07 2011-09-07 選択性ｃｏｘ−２阻害剤および一酸化窒素ドナーである１，５−ジアリール−２−アルキルピロール−３−置換ニトロエステル

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Country Link
US (1) US9162979B2 (it)
EP (1) EP2614050B1 (it)
JP (1) JP2013536876A (it)
CA (1) CA2808724A1 (it)
ES (1) ES2568253T3 (it)
IT (1) IT1402177B1 (it)
WO (1) WO2012032479A1 (it)

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2006099416A1 (en) * 2005-03-11 2006-09-21 Nitromed, Inc. 2-methyl indole cyclooxygenase-2 selective inhibitors, compositions and methods of use
JP2009545539A (ja) * 2006-08-03 2009-12-24 ロッタファルム・ソシエタ・ペル・アチオニ 高選択性および経口有効性ｃｏｘ−２インヒビターである３−置換−１，５−ジアリール−２−アルキルピロール

Family Cites Families (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
IT1256450B (it) 1992-11-26 1995-12-05 Soldato Piero Del Esteri nitrici con attivita' farmacologica e procedimento per la loro preparazione
WO1995009831A1 (en) 1993-10-06 1995-04-13 Nicox S.A. Nitric esters having anti-inflammatory and/or analgesic activity and process for their preparation
JP2003523958A (ja) * 1999-12-23 2003-08-12 ニトロメド インコーポレーテッド ニトロソ化およびニトロシル化されたシクロオキシゲナーゼ−２の阻害剤、組成物ならびに使用法
JP2007520483A (ja) 2004-01-27 2007-07-26 メルク フロスト カンパニー シクロオキシゲナーゼ−２インヒビターとしてのジアリール−２−（５ｈ）−フラノンの一酸化窒素放出プロドラッグ
CA2683488A1 (en) 2007-04-25 2008-11-06 Nicox S.A. Use of 4-(nitrooxy)-butyl-(s)-2-(6-methoxy-2-naphtyl)-propanoate for treating pain and inflammation

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2006099416A1 (en) * 2005-03-11 2006-09-21 Nitromed, Inc. 2-methyl indole cyclooxygenase-2 selective inhibitors, compositions and methods of use
JP2009545539A (ja) * 2006-08-03 2009-12-24 ロッタファルム・ソシエタ・ペル・アチオニ 高選択性および経口有効性ｃｏｘ−２インヒビターである３−置換−１，５−ジアリール−２−アルキルピロール

Non-Patent Citations (2)

* Cited by examiner, † Cited by third party
Title
JPN6015021102; Ｗｅｙ，　Ｓ-Ｊ．　ｅｔ　ａｌ: Ｊｏｕｒｎａｌ　ｏｆ　Ｍｅｄｉｃｉｎａｌ　Ｃｈｅｍｉｓｔｒｙ ｖｏｌ．　５０　ｎｏ．　２５, 2007, ｐ．　６３６７-６３８２ *
JPN6015021104; Ａｂｄｅｌｌａｔｉｆ，　Ｋ．Ｒ．Ａ．　ｅｔ　ａｌ: Ｂｉｏｏｒｇ．　Ｍｅｄ．　Ｃｈｅｍ．　Ｌｅｔｔ． ｖｏｌ．　１９, 2009, ｐ．　３０１４-３０１８ *

Also Published As

Publication number Publication date
EP2614050A1 (en) 2013-07-17
IT1402177B1 (it) 2013-08-28
ES2568253T3 (es) 2016-04-28
CA2808724A1 (en) 2012-03-15
US9162979B2 (en) 2015-10-20
WO2012032479A1 (en) 2012-03-15
EP2614050B1 (en) 2016-01-20
WO2012032479A8 (en) 2012-07-12
US20130165494A1 (en) 2013-06-27
ITTO20100739A1 (it) 2012-03-08

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